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Cediranib Maleate

Name: Cediranib Maleate
Brand: Selleck Chemicals
SKU: S5242
Rating: 5 (14 reviews)

Synonyms: AZD2171 maleate

Catalog No.S5242 Purity: 99.93%

Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.

Cediranib Maleate Chemical Structure

CAS: 857036-77-2

Selleck's Cediranib Maleate has been cited by 14 publications

Purity & Quality Control

Batch: S524201 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.93%

99.93

Cediranib Maleate Related Products

Related Targets	VEGFR1 VEGFR2 VEGFR3	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	Click to Expand

Signaling Pathway

VEGFR Signaling Pathway

Choose Selective VEGFR Inhibitors

Biological Activity

Description

Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.

Targets

VEGFR2/KDR ^[2] (HUVECs)	c-Kit ^[2] (HUVECs)	c-Kit ^[2] (HUVECs)	VEGFR3/FLT4 ^[2] (HUVECs)	VEGFR1/FLT1 ^[2] (HUVECs)	Click to View More Targets
0.5 nM	2 nM	2 nM	<=3 nM	5 nM	Click to View More Targets

In vitro
In vitro	In recombinant kinase assays, cediranib inhibits VEGFR-1 kinase activity (IC50 = 5 nmol/L) within a similar concentration range to VEGFR-2 and VEGFR-3 (IC50 values of <0.1 and ≤3 nmol/L). It shows selectivity against other kinases. Cediranib has similar potency against c-Kit when compared with VEGFR-2 in phosphorylation assays but less potency against PDGFR-α and PDGFR-β, particularly in a PDGF-AA/PDGFR-α–driven tumor cell proliferation assay. Cediranib is inactive against wild-type Flt-3 (IC50 value >1 μmol/L) and had marginal activity versus FGFR-1 and -4 (IC50 values of 0.35 and 2.17 μmol/L, respectively)^[1].

In Vivo
In vivo	Phosphorylation of wild-type c-Kit in NCI-H526 tumor xenografts was reduced markedly following oral administration of cediranib (≥1.5 mg/kg/d) to tumor-bearing nude mice^[1].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT00458731	Completed	Adult Grade III Lymphomatoid Granulomatosis\|Adult Nasal Type Extranodal NK/T-cell Lymphoma\|Anaplastic Large Cell Lymphoma\|Angioimmunoblastic T-cell Lymphoma\|Childhood Burkitt Lymphoma\|Childhood Diffuse Large Cell Lymphoma\|Childhood Grade III Lymphomatoid Granulomatosis\|Childhood Immunoblastic Large Cell Lymphoma\|Childhood Nasal Type Extranodal NK/T-cell Lymphoma\|Cutaneous B-cell Non-Hodgkin Lymphoma\|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue\|Hepatosplenic T-cell Lymphoma\|Intraocular Lymphoma\|Nodal Marginal Zone B-cell Lymphoma\|Noncutaneous Extranodal Lymphoma\|Peripheral T-cell Lymphoma\|Progressive Hairy Cell Leukemia Initial Treatment\|Recurrent Adult Burkitt Lymphoma\|Recurrent Adult Diffuse Large Cell Lymphoma\|Recurrent Adult Diffuse Mixed Cell Lymphoma\|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma\|Recurrent Adult Hodgkin Lymphoma\|Recurrent Adult Immunoblastic Large Cell Lymphoma\|Recurrent Adult Lymphoblastic Lymphoma\|Recurrent Adult T-cell Leukemia/Lymphoma\|Recurrent Childhood Anaplastic Large Cell Lymphoma\|Recurrent Childhood Large Cell Lymphoma\|Recurrent Childhood Lymphoblastic Lymphoma\|Recurrent Childhood Small Noncleaved Cell Lymphoma\|Recurrent Grade 1 Follicular Lymphoma\|Recurrent Grade 2 Follicular Lymphoma\|Recurrent Grade 3 Follicular Lymphoma\|Recurrent Mantle Cell Lymphoma\|Recurrent Mycosis Fungoides/Sezary Syndrome\|Recurrent/Refractory Childhood Hodgkin Lymphoma\|Refractory Hairy Cell Leukemia\|Small Intestine Lymphoma\|Splenic Marginal Zone Lymphoma\|Stage IV Adult Burkitt Lymphoma\|Stage IV Adult Diffuse Large Cell Lymphoma\|Stage IV Adult Diffuse Mixed Cell Lymphoma\|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma\|Stage IV Adult Hodgkin Lymphoma\|Stage IV Adult Immunoblastic Large Cell Lymphoma\|Stage IV Adult Lymphoblastic Lymphoma\|Stage IV Adult T-cell Leukemia/Lymphoma\|Stage IV Childhood Anaplastic Large Cell Lymphoma\|Stage IV Childhood Hodgkin Lymphoma\|Stage IV Childhood Large Cell Lymphoma\|Stage IV Childhood Lymphoblastic Lymphoma\|Stage IV Childhood Small Noncleaved Cell Lymphoma\|Stage IV Grade 1 Follicular Lymphoma\|Stage IV Grade 2 Follicular Lymphoma\|Stage IV Grade 3 Follicular Lymphoma\|Stage IV Mantle Cell Lymphoma\|Stage IVA Mycosis Fungoides/Sezary Syndrome\|Stage IVB Mycosis Fungoides/Sezary Syndrome\|T-cell Large Granular Lymphocyte Leukemia\|Testicular Lymphoma\|Unspecified Adult Solid Tumor Protocol Specific\|Unspecified Childhood Solid Tumor Protocol Specific\|Waldenström Macroglobulinemia	National Cancer Institute (NCI)	May 2007	Phase 1

References

Chemical Information & Solubility

Molecular Weight	566.58	Formula	C₂₅H₂₇FN₄O₃.C₄H₄O₄
CAS No.	857036-77-2	SDF	--
Smiles	CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (176.49 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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